葡甘聚糖片段-环二肽协同降胆固醇作用及其构效关系研究

项目名称： 葡甘聚糖片段-环二肽协同降胆固醇作用及其构效关系研究

项目编号： No.31201350

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 膳食与营养

项目作者： 陈继承

作者单位： 福建农林大学

项目金额： 23万元

中文摘要： 本项目以葡甘聚糖片段和环二肽为原料，在电场作用下制备小分子糖肽复合物，研究复合物降胆固醇的作用机理并探索其构效关系。葡甘聚糖片段与环二肽在高压脉冲电场作用下制备小分子糖肽复合物；通过离子交换、制备液相色谱等现代纯化技术对复合物进行分离纯化得到不同的稳定组分；利用前期研究建立的降胆固醇成分筛选平台对不同组分进行活性筛选，确定不同糖肽复合物降胆固醇活性的差异，筛选出高活性的糖肽复合物；对比分析葡甘聚糖片段、环二肽及不同糖肽复合物降胆固醇活性和作用机理；最后利用红外、核磁共振、质谱等光谱分析技术对筛选出的糖肽复合物进行结构表征，结合分子模拟技术研究糖肽分子间相互作用方式、位点对其功能的影响机制，揭示构效关系。项目实施有望深入揭示小分子糖肽复合物中非共价键的相互作用方式、位点及其对降胆固醇活性的影响机制。在研究糖肽复合物构象稳定性与生物活性相关性方面具有重要的理论价值。

中文关键词： 环二肽；小分子糖肽；降胆固醇；构效关系；机理

英文摘要： Taking glucomannan fragments and cyclic dipeptide as the research objects, the oligosaccharides-peptide complexes were prepared in the electric field. The hypocholesterolemic mechanism and structure-activity relationships were investigated on them. The glucomannan fragments and cyclic dipeptide formed the small molecular complexes by high intensity pulsed electric field, and then the various components of products were separated and purified by the ionic exchange and preparative liquid chromatography. The hypocholesterolemic activity screening in vitro were performed to confirm the diversity of different complexes and to choose the complexes with high activity by the methods in our prophase research. The hypocholesterolemic effects and mechanism of the complexes were compared to the glucomannan fragments and cyclic dipeptide. Finally, the complexes were characterized by IR, NMR and MS analysis. Furthermore, armed with molecular simulation technology, we try to investigate the mode and sites of intermolecular action affecting on the hypocholesterolemic activity and then find out the structure-activity relationships. This study aims to reveal the interaction mode and primary site of non-covalent bond of complexes and the influence mechanism on hypocholesterolemic activity. These results would provide theoretical

英文关键词： Cyclic dipeptide； Small Glycopeptide；Hypocholesterolemic Effect；Structure-activity relationship；Mechanism